Abstract: The present invention provides compounds of formula (I) wherein R1, R2, R3, R4 and Q have a meaning as defined herein in the specification. The compounds of formula (I) are allosteric modulators of the A1 adenosine receptor and, thus, may be employed for the treatment of conditions mediated by the A1 adenosine receptor. Accordingly, the compounds of formula (I) may be employed for treatment of pain, in particular, chronic pain such as neuropathic pain; cardiac disease or disorder such as cardiac disarrhythmias, e.g., peroxysmal supraventricular tachycardia, angina, myocardial infarction and stroke; neurological disease or injury; sleep disorder; epilepsy; and depression.

Abstract: The present invention provides compounds of formula (I) wherein R1, R2, R3, R4 and Q have a meaning as defined herein in the specification. The compounds of formula (I) are allosteric modulators of the A1 adenosine receptor and, thus, may be employed for the treatment of conditions mediated by the A1 adenosine receptor. Accordingly, the compounds of formula (I) may be employed for treatment of pain, in particular, chronic pain such as neuropathic pain; cardiac disease or disorder such as cardiac disarrhythmias, e.g., peroxysmal supraventricular tachycardia, angina, myocardial infarction and stroke; neurological disease or injury; sleep disorder; epilepsy; and depression.

Abstract: The Wnt signaling pathways are involved in embryo development as well as in tumorigenesis. Dishevelled (Dvl) tranduces Wnt signals from the receptor Frizzled (Fz) to downstream components in canonical and non-canonical Wnt signaling pathways, and the Dvl PDZ domain plays an essential role in both pathways, and the Dvl PDZ domain binds directly to Fz receptors. In the present invention using NMR-assisted virtual ligand screening, several compounds were identified and were found to bind to the Dvl PDZ domain. Molecular dynamics simulation was used to analyze the binding between the PDZ domain and these compounds in detail. These compounds provide a basis for rational design of high-affinity inhibitors of the PDZ domain, which can block Wnt signaling by interrupting the Fz-Dvl interaction.

Abstract: The present invention provides novel compounds and methods for using them to treat diseases with aminothiophene inhibitors of IKK-? phosphorylation of I?B. In so doing these aminothiophene inhibitors block pathological activation of transcription factor NF-?B in which diseases excessive activation of NF-?B is implicated.

Abstract: The invention relates to heteroaromatic carboxamides of formula (I), wherein A, R1, R2 and X are as defined in the specification, processes and intermediates used in their preparation, pharmaceutical compositions containing them and their use in therapy.

Abstract: A compound represented by the formula (1): wherein A is a nitrogen atom or CR4, B is an oxygen atom, a sulfur atom or NR9 (provided that when A is a nitrogen atom, B is not NH), R1 is a C2-14 aryl group, L1 is a bond, CR10R11, an oxygen atom, a sulfur atom or NR12, X is OR13 SR13 or NR14NR15, R2 is a hydrogen atom, a formyl group, a C1-10 alkyl group or the like, L2 is a bond or the like, L3 is a bond, CR17R18, an oxygen atom, a sulfur atom or NR19, L4 is a bond, CR20R21, an oxygen atom, a sulfur atom or NR22, Y is an oxygen atom, a sulfur atom or NR23, and R3 is a C2-14 aryl group, a tautomer, prodrug or pharmaceutically acceptable salt of the compound or a solvate thereof.

Abstract: The present invention is directed to a compound having the general structure of formula (1): useful for the treatment, prevention or amelioration of a CXCR1 or CXCR2 chemokine-mediated disease.

Abstract: Methods of treating or preventing a disease or disorder in a subject are provided by the present invention which include administering a composition including a therapeutically effective amount of a protein kinase C (PKC) zeta inhibitor. A disease or disorder treated or prevented by administration of a PKC zeta inhibitor is characterized by abnormal vascular permeability. Diseases or disorders treated or prevented by administration of a composition including a therapeutically effective amount of a PKC zeta inhibitor include cancer, an ischemic condition and microvascular complications of a systemic or local condition in the subject, such as diabetes and/or diabetic macular edema. Additionally, methods of inhibiting PKC zeta are provided which include incubating PKC zeta in vivo, in vitro and/or in silico with a PKC zeta inhibitor.

Abstract: The present invention provides novel compounds and methods for using them to treat diseases with aminothiophene inhibitors of IKK-? phosphorylation of I?B. In so doing these aminothiophene inhibitors block pathological activation of transcription factor NF-?B in which diseases excessive activation of NF-?B is implicated.

Abstract: A process for preparation of a compound of formula (I), or a salt thereof, both as individual isomer and as mixtures thereof, wherein each of A and B is independently aryl or heteroaryl optionally substituted with 1 to 4 substituents; and R and R1, which can be the same or different, are hydrogen, C1-C6 alkyl or an amino-protecting group; comprising the reaction of a compound (II) wherein A and B are as defined above, with a compound (III) wherein each of R and R1 is independently C1-C6 alkyl or an amino-protecting group; and X is a leaving group; in the presence of a basic agent; and, if desired the conversion of a compound (I) to another compound (I); and/or, if desired, the separation of an isomeric mixture of a compound (I) into the individual isomers; and/or, if desired, the conversion of a compound (I) to a salt thereof.

Abstract: This invention concerns N-(ortho phenylaminoaryl), N?-alkyl sulfamides which are inhibitors of MEK and are useful in the treatment of cancer and other hyperproliferative diseases.

Abstract: Novel compositions for the treatment of IRDS and ARDS are indicated which contain a compound of formula (I), in which R1 is hydrogen or 2-(2-hydroxyethoxy)ethyl and/or a pharmacologically tolerable salt of this compound and lung surfactant

Abstract: Substituted 3-(benzoylureido)thiophene derivatives, processes for preparing them and their use The invention relates to compounds of the formula I where the radicals are as defined, and their physiologically tolerated salts. The compounds are suitable, for example, as medicaments for preventing and treating type 2 diabetes.

Abstract: Thiophene derivatives are described herein. The described invention also includes methods of making such thiophene derivatives as well as methods of using the same in the treatment of diseases.

Abstract: Fatty acid amide hydrolase inhibitors of the Formula: are provided wherein X is NH, CH2, O, or S; Q is O or S; Z is O or N; R is an aromatic moiety selected from the group consisting of substituted or unsubstituted aryl; substituted or unsubstituted biphenylyl, substituted or unsubstituted naphthyl, and substituted or unsubstituted phenyl; substituted or unsubstituted terphenylyl; substituted or unsubstituted cycloalkyl, heteroaryl, or alkyl; and R1 and R2 are independently selected from the group consisting of H, substituted or unsubstituted alkyl, substituted or unsubstituted heteroalkyl, and substituted or unsubstituted phenyl, substituted or unsubstituted biphenylyl, substituted or unsubstituted aryl, and substituted or unsubstituted heteroaryl; with the proviso that if Z is O, one of R1 and R2 is absent, and that if Z is N, optionally R1 and R2 may optionally be taken together to form a substituted or unsubstituted N-heterocycle or substituted or unsubstituted heteroaryl with the N atom to which they

Abstract: The present invention provides novel compounds and methods for using them to treat diseases with aminothiophene inhibitors of IKK-? phosphorylation of I?B. In so doing these aminothiophene inhibitors block pathological activation of transcription factor NF-?B in which diseases excessive activation of NF-?B is implicated.

Abstract: The present invention relates to compounds of formula (I) wherein R1, R2, R3, R4 and n are as defined in the description and claims, and pharmaceutically acceptable salts thereof. The compounds are useful for the treatment and/or prophylaxis of diseases which are associated with the antagonism of the glucagon receptor, such as diabetes.

Abstract: The present invention provides novel compounds having a dual antagonistic activity against thromboxane A2 receptor and prostaglandin D2 receptor and pharmaceutical compositions comprising them. A compound of the formula (I): wherein R1 is —CH2—CH?CH—CH2—CH2—CH2—COOR2 or —CH?CH—CH2—CH2—CH2—COOR2; R2 is hydrogen or alkyl; m is 0 or 1; p is 0 or 1; X1 and X3 each is independently optionally substituted aryl or optionally substituted heteroaryl; X2 is a bond, —CH2—, —S—, —SO2—, —CH2—O—, —O—CH2—, —CH2—S—, —S—CH2—, or the like; X4 is —CH2—, —CH2—CH2—, —C(?O)—, or the like, have a dual antagonistic activity against both a thromboxane A2 receptor and a prostaglandin D2 receptor.

Abstract: The invention relates to thiophene carboxamides of formula (I), wherein R1, R2, R3, A, n and X are as defined in the specification, processes and intermediates used in their preparation, pharmaceutical compositions containing them and their use in therapy

Abstract: The present invention relates to a compound of formula (I): wherein: R3 is selected from the group consisting of 1-napthyl, 2-napthyl and cycloalkylphenyl; and R4 and R5 taken together form a ring having from 5 to 10 carbon atoms. Additionally, the invention provides a therapeutic method for preventing or treating a pathological condition or symptom in a mammal subject, such as a human, wherein increased angiogenesis is desired, comprising administering to a mammal in need of such therapy an effective amount of the aforementioned thiophene selective adenosine A1 allosteric enhancer.

Abstract: The invention provides a pharmaceutical for treatment of neurological and neuropsychiatric disorders comprising a compound of the formula: or a pharmaceutically acceptable salt thereof.

Abstract: The present invention is directed toward substituted hydroxyethylene compounds of formulas (XII) (XIII), and (XIV) useful in treating Alzheimer's disease and other similar diseases.

Abstract: The present invention relates to certain substituted polyketides of formula I, wherein A, B, C, D, E, F and m are as defined herein, pharmaceutical compositions containing said compounds, and the use of said compounds in treating tumors.

Abstract: The invention provides methods and compositions relating to novel pentafluorophenylsulfonamide derivatives and analogs and their use as pharmacologically active agents. The compositions find particular use as pharmacological agents in the treatment of disease states, particularly cancer, vascular restenosis, microbial infections, and psoriasis, or as lead compounds for the development of such agents.

Abstract: Disclosed are methods of treating certain cytokine mediated diseases or conditions using novel aromatic heterocyclic compounds of the formula(I) wherein Ar1,Ar2,L,Q and X are described herein.

Abstract: The present invention provides novel compounds represented by formula I: or pharmaceutically acceptable salts thereof useful for treating flaviviridae viral infection.

Abstract: The present invention relates to compounds of the formula I wherein A1, A2, R1, R2, R3, X and n are as defined in the claims, which are valuable pharmaceutically active compounds for the therapy and prophylaxis of diseases, for example of cardiovascular diseases such as hypertension, angina pectoris, cardiac insufficiency, thromboses or atherosclerosis. The compounds of the formula I are capable of modulating the body's production of cyclic guanosine monophosphate (cGMP) and are generally suitable for the therapy and prophylaxis of diseases which are associated with a disturbed cGMP balance. The invention furthermore relates to processes for preparing compounds of the formula I, to their use for the therapy and prophylaxis of the abovementioned diseases and for preparing pharmaceuticals for this purpose, and to pharmaceutical preparations which comprise compounds of the formula I.

Abstract: A composition comprising a combination of a compound of formula I in which R1 is hydrogen or 2-(2-hydroxyethoxy)ethyl and/or a pharmacologically tolerable salt thereof, and lung surfactant is useful for treating patients afflicted with IRDS or ARDS.

Abstract: An amine derivative, its tautomeric or stereoisomeric form, or a salt thereof which has vanilloid receptor 1 (VR1) antagonistic activity, is disclosed. The amine derivative has an excellent activity as VR1 antagonist and useful for the prophylaxis and treatment of diseases associated with VR1 activity, in particular for the treatment of urinary incontinence, overactive bladder, chronic pain, neuropathic pain, postoperative pain, rheumatoid arthritic pain, neuralgia, neuropathies, algesia, nerve injury, ischaemia, neurodegeneration, stroke, incontinence and/or inflammatory disorders.

Abstract: Infection by a Coronaviridae virus (e.g., a coronavirus) and/or illness due to a Coronaviridae virus are treated or protected against by administration of a therapeutically or prophylactically effective amount of certain nucleoside compounds and derivatives thereof, either alone or in a composition comprising the nucleoside compound or its derivative and a pharmaceutically acceptable carrier. In addition, replication of a Coronaviridae virus is inhibited by administration of the nucleoside compounds and derivatives thereof, either alone or in pharmaceutical compositions. The nucleosides are particularly suitable for use in treating or prophylaxis of an infection by the SARS virus and/or in treating or prophylaxis of SARS, and for use in inhibiting replication of the SARS virus. The nucleoside compounds and derivatives can optionally be administered in combination with other agents active against the Coronaviridae virus and/or an illness due to the virus.

Abstract: The invention relates to thiophene carboxanmides of formula (I). wherein A, R1, R2, R3, n and X are as defined in the specification, processes and intermediates used in their preparation, pharmaceutical compositions containing them and their use in therapy.

Abstract: A novel class of compounds, which act to antagonize the action of the glucagon hormone on the glucagon receptor. Owing to their antagonizing effect of the glucagon receptor the compounds may be suitable for the treatment and/or prevention of any diseases and disorders, wherein a glucagon antagonistic action is beneficial, such as hyperglycemia, Type 1 diabetes, Type 2 diabetes, disorders of the lipid metabolism and obesity.

Abstract: Compounds of the formula 1

Abstract: The present invention relates to compounds of formula (I) 1

Abstract: Substituted 3-(benzoylureido)thiophene derivatives, processes for preparing them and their use

Abstract: Novel compositions for the treatment of IRDS and ARDS are indicated which contain a compound of formula (I), in which R1 is hydrogen or 2-(2-hydroxyethoxy)ethyl and/or a pharmacologically tolerable salt of this compound and lung surfactant.

Abstract: The present invention provides compounds, compositions and methods for the selective inhibition of cathepsin S. In a preferred aspect, cathepsin S is selectively inhibited in the presence of at least one other cathepsin isozyme (e.g., cathespin K). The present invention also provides methods for treating a disease state in a subject by selectively inhibiting cathepsin S.

Abstract: A sulfonamide compound of the formula (I):

Abstract: The present invention relates to a compound of formula (I): 1

Abstract: Novel anthelmintic compositions containing thiophene derivatives as active ingredients are disclosed.

Abstract: The present invention provides novel compounds represented by formula I: 1

Abstract: Compounds of the formula I, 1

Abstract: This invention relates to the use of a group of aryl ureas in treating cytokine mediated diseases and proteolytic enzyme mediated diseases, and pharmaceutical compositions for use in such therapy.

Abstract: The present invention addresses substituted cyanothiophene derivatives of the formula I: 1

Abstract: The present invention addresses substituted cyanothiophene derivatives of the formula I: 1

Abstract: The invention encompasses nucleoside compounds, compositions comprising the compounds and methods for treating or preventing diseases associated with nonsense mutations of mRNA by administering these compounds or compositions.

Abstract: The present invention relates to compounds of the formula I, in which R1, R2, R4, R5, D1, D2, X1, X2, X3, A and B have the meanings indicated in the claims. The compounds of the formula I are valuable pharmacologically active compounds. They exhibit a strong antithrombotic effect and are suitable, for example, for the therapy and prophylaxis of thromboembolic diseases and restenoses. They are reversible inhibitors of the blood clotting enzyme factor VIIa and can in general be applied in conditions in which an undesired activity of factor VIIa is present or for the cure or prevention of which an inhibition of factor VIIa is intended. The invention furthermore relates to processes for the preparation of compounds of the formula I, their use, in particular as active ingredients in pharmaceuticals, and pharmaceutical preparations comprising them.

Abstract: A pharmaceutical composition comprising a pharmaceutically acceptable excipient and a compound of formula I: 1

Abstract: &agr;- and &bgr;-amino acid hydroxyethylamino sulfonamide compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease.

Abstract: The present invention provides novel compounds and methods for treating diseases with aminothiophene inhibitors of IKK-&bgr; phosphorylation of I&kgr;B.